Characterization of PCL and Chitosan Nanoparticles as Carriers of Enoxaparin and Its Antithrombotic Effect in Animal Models of Venous Thrombosis

Abstract

This study was based on the preparation, characterization, and animal in vivo experiments performed to evaluate nanoparticles of poly(ɛ-caprolactone) (PCL) and chitosan as carriers of enoxaparin. The nanoparticles were characterized and presented satisfactory results in terms of size, polydispersity, and encapsulation efficiency. Anticoagulant activity of the nanoparticles was maintained for 14 hours when the administration was subcutaneous; however no activity was observed after oral administration. There was a significant reduction in thrombus size, in vivo, for both free and encapsulated enoxaparin in comparison with the control group after subcutaneous administration. Oral administration results however were indifferent. In conclusion, the double emulsion method w/o/w was efficient for enoxaparin encapsulation, producing spherical nanoparticles with high encapsulation efficiency. For in vivo studies, the encapsulated enoxaparin showed a sustained anticoagulant activity for a higher period of time compared to free enoxaparin, with an antithrombotic effect when administered subcutaneously.

Production and characterization of low molecular weight heparin obtained by modified double emulsion method with solvent evaporation

“…As LMWH is hydrophilic, the literature reports that the encapsulation of this type of substance is complex, since there is a greater diffusion of the active to the external aqueous phase before the precipitation of the polymer, thus reducing the encapsulation efficiency. 7 In this study, the LMWH Encapsulation Efficiency was 66.5%, showing that despite the hydrophilic characteristics of the drug, the methodology employed in the development of the carrier system was satisfactory, a result similar to that obtained by Jogala et al, 2015 which obtained 46-70% EE, when nanoencapsular LMWH using PVA and PLGA9 double emulsion methodology. Thus, it can be stated that the EE obtained with the described methodology agrees with the literature and, therefore, satisfactory.…”

“…6 In the article by Prado LB et al, LMWH was nanoencapsulated using poly (E-caprolactone) (PCL) and chitosan and the results obtained were Dm 512.5nm, IPD 0.409 and PZ + 30.9mV of chitosan in the process. In this study the solvent-evaporated double emulsion method produced nanoparticles larger than 400nm and IPD greater than 0.2 characterizing system polydispersion, in other words, nanoparticles of varying sizes, 7 suggesting that the efficiency of developing a nanocarrier system is related to the methodology employed and the selected inputs.…”

Production and Characterization of Melon Sulfated Pectin (Cucumis melo var. acidulus) Nanoparticles with Anticoagulant Potential

“…10 In a similar test, medium-sized nanoparticles 512.8nm and 269nm were produced for nanoencapsulated low molecular weight heparin, using PVA and PLGA as well. 12,23 Regarding low PDI, the literature confirms that low values reveal good homogeneity of the samples. 21 Already analyzing the zeta potential, this parameter is probably related to the free carboxylic groups on the surface.…”

Low-Molecular-Weight Heparins: Reduced Size Particulate Systems for Improved Therapeutic Outcomes

“…Novel drug delivery systems have been explored globally for the last few decades; however, nanoparticles constitute the most extensively investigated tools, since they can be modified for their size, surface properties, and area to improve their solubility, retention time, and bioavailability [ 67 , 84 , 85 , 86 , 87 , 88 , 89 ]. Different sizes of these colloids can be prepared from a large number of polymers, surfactants, and dendrimers.…”